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View article: Synthesis of Diversely Substituted Diethyl (Pyrrolidin-2-Yl)Phosphonates
Synthesis of Diversely Substituted Diethyl (Pyrrolidin-2-Yl)Phosphonates Open
Imidazoline I2 receptors (I2-IR) are untapped therapeutic targets lacking a structural description. Although the levels of I2-IR are dysregulated in a plethora of illnesses, the arsenal of ligands that can modulate I2-IR is limited. In thi…
View article: Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2<i>H</i>-pyrrol-2-yl)phosphonates as Imidazoline <i>I</i><sub>2</sub> Receptor Ligands with Anti-Alzheimer and Analgesic Properties
Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2<i>H</i>-pyrrol-2-yl)phosphonates as Imidazoline <i>I</i><sub>2</sub> Receptor Ligands with Anti-Alzheimer and Analgesic Properties Open
Imidazoline I2 receptors (I2-IRs) are altered in Alzheimer's disease (AD) patients and are associated with analgesia. I2-IRs are not structurally described, and their pharmacological characterization relies on their modulation by highly af…
View article: CCDC 2250192: Experimental Crystal Structure Determination
CCDC 2250192: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2250190: Experimental Crystal Structure Determination
CCDC 2250190: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2250191: Experimental Crystal Structure Determination
CCDC 2250191: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2250189: Experimental Crystal Structure Determination
CCDC 2250189: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2250193: Experimental Crystal Structure Determination
CCDC 2250193: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: A bicyclic α‑iminophosphonate improves cognitive decline in 5xFAD murine model of neurodegeneration
A bicyclic α‑iminophosphonate improves cognitive decline in 5xFAD murine model of neurodegeneration Open
I 2 receptors (I 2 ‐IR) are widely distributed in the central nervous system. I 2 ‐IR ligands are associated with a neuroprotective effect but, as I 2 ‐IR structure remains unknown, the discovery of better and more selective ligands is nec…
View article: Synthesis, Characterization and HPLC Analysis of the (1S,2S,5R)-Diastereomer and the Enantiomer of the Clinical Candidate AR-15512
Synthesis, Characterization and HPLC Analysis of the (1S,2S,5R)-Diastereomer and the Enantiomer of the Clinical Candidate AR-15512 Open
AR-15512 (formerly known as AVX-012 and WS-12) is a TRPM8 receptor agonist currently in phase 2b clinical trials for the treatment of dry eye. This bioactive compound with menthol-like cooling activity has three stereogenic centers, and it…
View article: Rationally derived inhibitors of hepatitis C virus (HCV) p7 channel activity reveal prospect for bimodal antiviral therapy
Rationally derived inhibitors of hepatitis C virus (HCV) p7 channel activity reveal prospect for bimodal antiviral therapy Open
Since the 1960s, a single class of agent has been licensed targeting virus-encoded ion channels, or ‘viroporins’, contrasting the success of channel blocking drugs in other areas of medicine. Although resistance arose to these prototypic a…
View article: Author response: Rationally derived inhibitors of hepatitis C virus (HCV) p7 channel activity reveal prospect for bimodal antiviral therapy
Author response: Rationally derived inhibitors of hepatitis C virus (HCV) p7 channel activity reveal prospect for bimodal antiviral therapy Open
Article Figures and data Abstract Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract Since the 1960s, a single class of agent h…
View article: CCDC 1960885: Experimental Crystal Structure Determination
CCDC 1960885: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1960884: Experimental Crystal Structure Determination
CCDC 1960884: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1960883: Experimental Crystal Structure Determination
CCDC 1960883: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1960886: Experimental Crystal Structure Determination
CCDC 1960886: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1960887: Experimental Crystal Structure Determination
CCDC 1960887: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Bicyclic α‑Iminophosphonatesas HighAffinity Imidazoline I2 Receptor Ligands for Alzheimer’sDisease
Bicyclic α‑Iminophosphonatesas HighAffinity Imidazoline I2 Receptor Ligands for Alzheimer’sDisease Open
Imidazoline\nI2 receptors (I2-IR), widely\ndistributed in the CNS and altered in patients that suffer from neurodegenerative\ndisorders, are orphans from a structural point of view, and new I2-IR ligands are urgently required for improving…
View article: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I<sub>2</sub> Receptor Ligands for Alzheimer’s Disease
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I<sub>2</sub> Receptor Ligands for Alzheimer’s Disease Open
Imidazoline I2 receptors (I2-IR), widely distributed in the CNS and altered in patients that suffer from neurodegenerative disorders, are orphans from a structural point of view, and new I2-IR ligands are urgently required for improving th…
View article: Biological Evaluation of a Mitochondrial Phosphoenolpyruvate Carboxykinase Inhibitor
Biological Evaluation of a Mitochondrial Phosphoenolpyruvate Carboxykinase Inhibitor Open
Phosphoenolpyruvate carboxykinase (PEPCK) is a key enzyme in gluconeogenesis, catalyzingthe decarboxylation of oxaloacetate to phosphoenolpyruvate. [...]
View article: (2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together
(2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together Open
2-Imidazoline-containing compounds constitute a valuable class of agents that modulate α2-adrenergic receptors and often show a high affinity for imidazoline I2-receptors (I2-IR). [...]
View article: Dibenzylxanthines as PPEPCK-M Inhibitors for Cancer Therapy
Dibenzylxanthines as PPEPCK-M Inhibitors for Cancer Therapy Open
Phosphoenolpyruvate carboxykinase (PEPCK) is the key enzyme in gluconeogenesis/glyceroneogenesis, which catalyzes the decarboxylation of oxaloacetate to phosphoenolpyruvate. In eukaryotes, there are two isozymes present either in the cytos…
View article: CCDC 1576708: Experimental Crystal Structure Determination
CCDC 1576708: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …